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Updated: Jun 17, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
12:40

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

14.9K

FDA-approved small molecule kinase inhibitors for cancer treatment (2001-2015): Medical indication, structural

Ying Wang1, Xiang Nan2, Yanping Duan3

  • 1Department of Electrophysiological Diagnosis, 3201 Hospital of Xi'an Jiaotong University Health Science Center, Hanzhong 723000, China.

Bioorganic & Medicinal Chemistry
|August 11, 2024
PubMed

Insights

Kinase dysregulation drives cancer. This review updates medical uses, design, and binding of 28 FDA-approved small molecule kinase inhibitors (SMKIs) to guide future anticancer drug development.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Discovery

Background:

  • Kinase dysregulation is central to cancer development, progression, and metastasis.
  • Small molecule kinase inhibitors (SMKIs) represent a significant class of targeted anticancer therapies.
  • Twenty-eight SMKIs were approved by the FDA for cancer treatment by the end of 2015.

Purpose of the Study:

  • To provide an updated review of FDA-approved anti-tumor SMKIs.
  • To analyze their medical indications, design principles, and binding modes.
  • To offer insights for the future development of effective and safe SMKIs.

Main Methods:

  • Literature review of preclinical and clinical data for FDA-approved SMKIs.
  • Analysis of drug design strategies and molecular interactions.
  • Synthesis of information on medical applications and therapeutic outcomes.

Main Results:

  • Summary of current medical indications for 28 anti-tumor SMKIs.
  • Overview of key design principles and structure-activity relationships.
  • Detailed examination of binding modes and their impact on efficacy and safety.

Conclusions:

  • Updated understanding of approved SMKIs is crucial for advancing cancer therapy.
  • Insights into design and binding modes can inform the development of next-generation SMKIs.
  • Future SMKIs should prioritize specific efficacy and improved safety profiles.
Keywords:
Binding modeCancerMedical indicationOptimization principleProtein kinases

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